TW202313038A - 用於治療晚期實性瘤之fgfr酪胺酸激酶抑制劑 - Google Patents
用於治療晚期實性瘤之fgfr酪胺酸激酶抑制劑 Download PDFInfo
- Publication number
- TW202313038A TW202313038A TW111118772A TW111118772A TW202313038A TW 202313038 A TW202313038 A TW 202313038A TW 111118772 A TW111118772 A TW 111118772A TW 111118772 A TW111118772 A TW 111118772A TW 202313038 A TW202313038 A TW 202313038A
- Authority
- TW
- Taiwan
- Prior art keywords
- fgfr2
- cancer
- fgfr
- carcinoma
- fgfr3
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims description 73
- 208000037844 advanced solid tumor Diseases 0.000 title description 13
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- 108091008794 FGF receptors Proteins 0.000 claims abstract description 801
- 102000044168 Fibroblast Growth Factor Receptor Human genes 0.000 claims abstract description 800
- 230000004927 fusion Effects 0.000 claims abstract description 431
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 372
- 201000011510 cancer Diseases 0.000 claims abstract description 329
- 229950004444 erdafitinib Drugs 0.000 claims abstract description 211
- OLAHOMJCDNXHFI-UHFFFAOYSA-N n'-(3,5-dimethoxyphenyl)-n'-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-n-propan-2-ylethane-1,2-diamine Chemical compound COC1=CC(OC)=CC(N(CCNC(C)C)C=2C=C3N=C(C=NC3=CC=2)C2=CN(C)N=C2)=C1 OLAHOMJCDNXHFI-UHFFFAOYSA-N 0.000 claims abstract description 211
- 238000000034 method Methods 0.000 claims abstract description 207
- 229940125829 fibroblast growth factor receptor inhibitor Drugs 0.000 claims abstract description 203
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims abstract description 135
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims abstract description 135
- 210000004027 cell Anatomy 0.000 claims abstract description 117
- 208000029824 high grade glioma Diseases 0.000 claims abstract description 83
- 201000011614 malignant glioma Diseases 0.000 claims abstract description 83
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims abstract description 82
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims abstract description 82
- 201000002528 pancreatic cancer Diseases 0.000 claims abstract description 82
- 208000008443 pancreatic carcinoma Diseases 0.000 claims abstract description 82
- 208000006990 cholangiocarcinoma Diseases 0.000 claims abstract description 81
- 206010033128 Ovarian cancer Diseases 0.000 claims abstract description 80
- 206010061535 Ovarian neoplasm Diseases 0.000 claims abstract description 80
- 208000030173 low grade glioma Diseases 0.000 claims abstract description 77
- 201000008443 lung non-squamous non-small cell carcinoma Diseases 0.000 claims abstract description 77
- 206010006187 Breast cancer Diseases 0.000 claims abstract description 74
- 208000026310 Breast neoplasm Diseases 0.000 claims abstract description 74
- 206010014733 Endometrial cancer Diseases 0.000 claims abstract description 73
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims abstract description 73
- 206010061934 Salivary gland cancer Diseases 0.000 claims abstract description 73
- 206010014759 Endometrial neoplasm Diseases 0.000 claims abstract description 72
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims abstract description 71
- 201000004101 esophageal cancer Diseases 0.000 claims abstract description 71
- 201000010536 head and neck cancer Diseases 0.000 claims abstract description 71
- 208000014829 head and neck neoplasm Diseases 0.000 claims abstract description 71
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims abstract description 66
- 206010004146 Basal cell carcinoma Diseases 0.000 claims abstract description 47
- 206010009944 Colon cancer Diseases 0.000 claims abstract description 47
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims abstract description 47
- 208000000821 Parathyroid Neoplasms Diseases 0.000 claims abstract description 47
- 206010060862 Prostate cancer Diseases 0.000 claims abstract description 47
- 208000005718 Stomach Neoplasms Diseases 0.000 claims abstract description 47
- 206010017758 gastric cancer Diseases 0.000 claims abstract description 47
- 201000011549 stomach cancer Diseases 0.000 claims abstract description 47
- 206010008342 Cervix carcinoma Diseases 0.000 claims abstract description 46
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims abstract description 46
- 201000010881 cervical cancer Diseases 0.000 claims abstract description 46
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims abstract description 45
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims abstract description 43
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims abstract description 43
- 201000003913 parathyroid carcinoma Diseases 0.000 claims abstract description 37
- 208000017954 parathyroid gland carcinoma Diseases 0.000 claims abstract description 37
- 101150081124 FGFR gene Proteins 0.000 claims abstract description 25
- 239000012472 biological sample Substances 0.000 claims abstract description 24
- 239000000523 sample Substances 0.000 claims abstract description 24
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims abstract description 20
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims abstract description 20
- 206010073373 small intestine adenocarcinoma Diseases 0.000 claims abstract description 20
- 206010073087 Malignant sweat gland neoplasm Diseases 0.000 claims abstract description 19
- 201000000281 malignant syringoma Diseases 0.000 claims abstract description 19
- 230000010558 Gene Alterations Effects 0.000 claims abstract description 18
- 230000004077 genetic alteration Effects 0.000 claims description 243
- 231100000118 genetic alteration Toxicity 0.000 claims description 243
- 230000035772 mutation Effects 0.000 claims description 226
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims description 100
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims description 99
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims description 84
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims description 84
- 201000009030 Carcinoma Diseases 0.000 claims description 70
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims description 61
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims description 60
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims description 60
- 206010054184 Small intestine carcinoma Diseases 0.000 claims description 52
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 52
- 201000002510 thyroid cancer Diseases 0.000 claims description 52
- 201000009365 Thymic carcinoma Diseases 0.000 claims description 44
- 208000008732 thymoma Diseases 0.000 claims description 37
- 239000003814 drug Substances 0.000 claims description 35
- 206010061825 Duodenal neoplasm Diseases 0.000 claims description 30
- 201000000312 duodenum cancer Diseases 0.000 claims description 30
- 102220198172 rs121913474 Human genes 0.000 claims description 29
- 102200126674 rs121913478 Human genes 0.000 claims description 29
- 102200143266 rs121913483 Human genes 0.000 claims description 28
- 206010027406 Mesothelioma Diseases 0.000 claims description 26
- 206010039491 Sarcoma Diseases 0.000 claims description 26
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims description 26
- 201000002547 conjunctival squamous cell carcinoma Diseases 0.000 claims description 26
- 201000010175 gallbladder cancer Diseases 0.000 claims description 26
- 230000003211 malignant effect Effects 0.000 claims description 26
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims description 25
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims description 25
- 201000008170 anus adenocarcinoma Diseases 0.000 claims description 25
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims description 25
- 208000021309 Germ cell tumor Diseases 0.000 claims description 23
- 208000025106 carcinoma of duodenum Diseases 0.000 claims description 22
- 201000007487 gallbladder carcinoma Diseases 0.000 claims description 22
- 102200143269 rs121913482 Human genes 0.000 claims description 21
- 102200127024 rs869320694 Human genes 0.000 claims description 18
- 230000002381 testicular Effects 0.000 claims description 15
- 208000033781 Thyroid carcinoma Diseases 0.000 claims description 14
- 102200126949 rs121918505 Human genes 0.000 claims description 14
- 208000013077 thyroid gland carcinoma Diseases 0.000 claims description 14
- 102200126910 rs79184941 Human genes 0.000 claims description 13
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 12
- 206010057644 Testis cancer Diseases 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 12
- 102200126596 rs121918506 Human genes 0.000 claims description 12
- 201000003120 testicular cancer Diseases 0.000 claims description 12
- 102200143278 rs17881656 Human genes 0.000 claims description 10
- 210000004430 acanthocyte Anatomy 0.000 claims description 8
- 102200125620 rs121913473 Human genes 0.000 claims description 6
- 102200143267 rs4647924 Human genes 0.000 claims description 6
- 238000009121 systemic therapy Methods 0.000 claims description 5
- 101001091968 Homo sapiens Rhophilin-2 Proteins 0.000 claims description 4
- 102100035749 Rhophilin-2 Human genes 0.000 claims description 4
- 239000007909 solid dosage form Substances 0.000 claims description 4
- 210000004369 blood Anatomy 0.000 claims description 3
- 239000008280 blood Substances 0.000 claims description 3
- 210000001185 bone marrow Anatomy 0.000 claims description 3
- 239000000969 carrier Substances 0.000 claims description 3
- 210000004880 lymph fluid Anatomy 0.000 claims description 3
- 101001064097 Homo sapiens Protein disulfide-thiol oxidoreductase Proteins 0.000 claims description 2
- 102100030734 Protein disulfide-thiol oxidoreductase Human genes 0.000 claims description 2
- 230000002496 gastric effect Effects 0.000 claims description 2
- 102100020976 G kinase-anchoring protein 1 Human genes 0.000 claims 1
- 101001075222 Homo sapiens G kinase-anchoring protein 1 Proteins 0.000 claims 1
- 101001056627 Homo sapiens Janus kinase and microtubule-interacting protein 1 Proteins 0.000 claims 1
- 102100025834 Janus kinase and microtubule-interacting protein 1 Human genes 0.000 claims 1
- YPIQVCUJEKAZCP-UHFFFAOYSA-N Malotilate Chemical compound CC(C)OC(=O)C(C(=O)OC(C)C)=C1SC=CS1 YPIQVCUJEKAZCP-UHFFFAOYSA-N 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 208000000728 Thymus Neoplasms Diseases 0.000 abstract description 10
- 206010041823 squamous cell carcinoma Diseases 0.000 abstract 1
- 230000004044 response Effects 0.000 description 85
- 238000012552 review Methods 0.000 description 40
- 239000003112 inhibitor Substances 0.000 description 35
- 201000010099 disease Diseases 0.000 description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 22
- 150000003839 salts Chemical class 0.000 description 21
- 239000012453 solvate Substances 0.000 description 21
- 108090000623 proteins and genes Proteins 0.000 description 15
- 208000005017 glioblastoma Diseases 0.000 description 12
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 11
- 229940124597 therapeutic agent Drugs 0.000 description 11
- 201000010915 Glioblastoma multiforme Diseases 0.000 description 10
- 239000002585 base Substances 0.000 description 10
- 150000001875 compounds Chemical class 0.000 description 10
- 229940079593 drug Drugs 0.000 description 10
- 208000026045 malignant tumor of parathyroid gland Diseases 0.000 description 10
- 150000001204 N-oxides Chemical class 0.000 description 9
- 201000009377 thymus cancer Diseases 0.000 description 9
- 102000018233 Fibroblast Growth Factor Human genes 0.000 description 7
- 108050007372 Fibroblast Growth Factor Proteins 0.000 description 7
- 239000002253 acid Substances 0.000 description 7
- 230000004075 alteration Effects 0.000 description 7
- 229940126864 fibroblast growth factor Drugs 0.000 description 7
- 201000003804 salivary gland carcinoma Diseases 0.000 description 7
- 206010003571 Astrocytoma Diseases 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 230000003389 potentiating effect Effects 0.000 description 6
- 102100036783 Arf-GAP with GTPase, ANK repeat and PH domain-containing protein 1 Human genes 0.000 description 5
- CUDVHEFYRIWYQD-UHFFFAOYSA-N E-3810 free base Chemical group C=1C=C2C(C(=O)NC)=CC=CC2=CC=1OC(C1=CC=2OC)=CC=NC1=CC=2OCC1(N)CC1 CUDVHEFYRIWYQD-UHFFFAOYSA-N 0.000 description 5
- 208000006168 Ewing Sarcoma Diseases 0.000 description 5
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 description 5
- 208000032612 Glial tumor Diseases 0.000 description 5
- 206010018338 Glioma Diseases 0.000 description 5
- 101000928218 Homo sapiens Arf-GAP with GTPase, ANK repeat and PH domain-containing protein 1 Proteins 0.000 description 5
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 description 5
- 208000000172 Medulloblastoma Diseases 0.000 description 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 5
- 206010029260 Neuroblastoma Diseases 0.000 description 5
- 208000008383 Wilms tumor Diseases 0.000 description 5
- 230000000259 anti-tumor effect Effects 0.000 description 5
- 230000008901 benefit Effects 0.000 description 5
- 239000002773 nucleotide Substances 0.000 description 5
- 125000003729 nucleotide group Chemical group 0.000 description 5
- 201000009410 rhabdomyosarcoma Diseases 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 4
- 208000022072 Gallbladder Neoplasms Diseases 0.000 description 4
- 101000577335 Homo sapiens Nuclear receptor-binding factor 2 Proteins 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 102100028791 Nuclear receptor-binding factor 2 Human genes 0.000 description 4
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 4
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 4
- 235000011054 acetic acid Nutrition 0.000 description 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 4
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 description 4
- 230000002285 radioactive effect Effects 0.000 description 4
- 208000011580 syndromic disease Diseases 0.000 description 4
- KEIPNCCJPRMIAX-HNNXBMFYSA-N 1-[(3s)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one Chemical compound COC1=CC(OC)=CC(C#CC=2C3=C(N)N=CN=C3N([C@@H]3CN(CC3)C(=O)C=C)N=2)=C1 KEIPNCCJPRMIAX-HNNXBMFYSA-N 0.000 description 3
- HNLRRJSKGXOYNO-UHFFFAOYSA-N 4-[[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl]piperazin-2-one Chemical compound N12N=CN=C(N)C2=C(C=2SC3=C(OC)C=C(C)C=C3C=2)C(COC)=C1CN1CCNC(=O)C1 HNLRRJSKGXOYNO-UHFFFAOYSA-N 0.000 description 3
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 108090000386 Fibroblast Growth Factor 1 Proteins 0.000 description 3
- 108090000379 Fibroblast growth factor 2 Proteins 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 201000007286 Pilocytic astrocytoma Diseases 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 3
- 150000007513 acids Chemical class 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 230000002068 genetic effect Effects 0.000 description 3
- 238000000746 purification Methods 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
- -1 3,5-dimethoxyphenyl Chemical group 0.000 description 2
- HCDMJFOHIXMBOV-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1CN1CCOCC1 HCDMJFOHIXMBOV-UHFFFAOYSA-N 0.000 description 2
- 206010060933 Adverse event Diseases 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- QADPYRIHXKWUSV-UHFFFAOYSA-N BGJ-398 Chemical compound C1CN(CC)CCN1C(C=C1)=CC=C1NC1=CC(N(C)C(=O)NC=2C(=C(OC)C=C(OC)C=2Cl)Cl)=NC=N1 QADPYRIHXKWUSV-UHFFFAOYSA-N 0.000 description 2
- 206010004593 Bile duct cancer Diseases 0.000 description 2
- 208000017897 Carcinoma of esophagus Diseases 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- 101150025764 FGFR3 gene Proteins 0.000 description 2
- 102000003971 Fibroblast Growth Factor 1 Human genes 0.000 description 2
- 102000003974 Fibroblast growth factor 2 Human genes 0.000 description 2
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 101001074975 Homo sapiens Molybdopterin molybdenumtransferase Proteins 0.000 description 2
- 101000588964 Homo sapiens Myosin-14 Proteins 0.000 description 2
- 101000958744 Homo sapiens Myosin-7B Proteins 0.000 description 2
- 101000613565 Homo sapiens PRKC apoptosis WT1 regulator protein Proteins 0.000 description 2
- 101000659053 Homo sapiens Synaptopodin-2 Proteins 0.000 description 2
- 101000763487 Homo sapiens Transmembrane protein 247 Proteins 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 2
- 238000005004 MAS NMR spectroscopy Methods 0.000 description 2
- 102100035971 Molybdopterin molybdenumtransferase Human genes 0.000 description 2
- 102100032972 Myosin-14 Human genes 0.000 description 2
- 238000005481 NMR spectroscopy Methods 0.000 description 2
- 102100040853 PRKC apoptosis WT1 regulator protein Human genes 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 229940124639 Selective inhibitor Drugs 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- 102100035603 Synaptopodin-2 Human genes 0.000 description 2
- 102100027013 Transmembrane protein 247 Human genes 0.000 description 2
- 108091008605 VEGF receptors Proteins 0.000 description 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 230000005856 abnormality Effects 0.000 description 2
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- IAJILQKETJEXLJ-QTBDOELSSA-N aldehydo-D-glucuronic acid Chemical compound O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C(O)=O IAJILQKETJEXLJ-QTBDOELSSA-N 0.000 description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 2
- 210000000436 anus Anatomy 0.000 description 2
- 230000003305 autocrine Effects 0.000 description 2
- 201000007180 bile duct carcinoma Diseases 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000002512 chemotherapy Methods 0.000 description 2
- 235000015165 citric acid Nutrition 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 2
- 229940125436 dual inhibitor Drugs 0.000 description 2
- 201000005619 esophageal carcinoma Diseases 0.000 description 2
- 239000001530 fumaric acid Substances 0.000 description 2
- 229940121446 futibatinib Drugs 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 229940097043 glucuronic acid Drugs 0.000 description 2
- 201000003911 head and neck carcinoma Diseases 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000002427 irreversible effect Effects 0.000 description 2
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 description 2
- 238000002955 isolation Methods 0.000 description 2
- 229960000448 lactic acid Drugs 0.000 description 2
- 229940098779 methanesulfonic acid Drugs 0.000 description 2
- 230000002018 overexpression Effects 0.000 description 2
- 229910052697 platinum Inorganic materials 0.000 description 2
- 230000035755 proliferation Effects 0.000 description 2
- 201000001514 prostate carcinoma Diseases 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 229950010624 rogaratinib Drugs 0.000 description 2
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 description 2
- 238000012163 sequencing technique Methods 0.000 description 2
- 230000011664 signaling Effects 0.000 description 2
- 238000000371 solid-state nuclear magnetic resonance spectroscopy Methods 0.000 description 2
- 230000004083 survival effect Effects 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 238000002411 thermogravimetry Methods 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 2
- KCOYQXZDFIIGCY-CZIZESTLSA-N (3e)-4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1,3-dihydrobenzimidazol-2-ylidene]quinolin-2-one Chemical compound C1CN(C)CCN1C1=CC=C(N\C(N2)=C/3C(=C4C(F)=CC=CC4=NC\3=O)N)C2=C1 KCOYQXZDFIIGCY-CZIZESTLSA-N 0.000 description 1
- KPJDVVCDVBFRMU-AREMUKBSSA-N (6r)-6-(2-fluorophenyl)-n-[3-[2-(2-methoxyethylamino)ethyl]phenyl]-5,6-dihydrobenzo[h]quinazolin-2-amine Chemical compound COCCNCCC1=CC=CC(NC=2N=C3C4=CC=CC=C4[C@H](C=4C(=CC=CC=4)F)CC3=CN=2)=C1 KPJDVVCDVBFRMU-AREMUKBSSA-N 0.000 description 1
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- SXAJXHQRSSZHPP-UHFFFAOYSA-N 1h-pyrido[4,3-d]pyrimidin-2-one Chemical compound N1=CC=C2NC(=O)N=CC2=C1 SXAJXHQRSSZHPP-UHFFFAOYSA-N 0.000 description 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 description 1
- VDZZYOJYLLNBTD-UHFFFAOYSA-N 2-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]pyrazol-1-yl]ethanol Chemical compound COC1=CC(OC)=C(F)C(COC=2C=NC(NC3=CN(CCO)N=C3)=NC=2)=C1F VDZZYOJYLLNBTD-UHFFFAOYSA-N 0.000 description 1
- UOQHWNPVNXSDDO-UHFFFAOYSA-N 3-bromoimidazo[1,2-a]pyridine-6-carbonitrile Chemical compound C1=CC(C#N)=CN2C(Br)=CN=C21 UOQHWNPVNXSDDO-UHFFFAOYSA-N 0.000 description 1
- 229940126287 ASP5878 Drugs 0.000 description 1
- 241000321096 Adenoides Species 0.000 description 1
- 102100040539 BTB/POZ domain-containing protein KCTD1 Human genes 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 102100033685 Cilia- and flagella-associated protein 58 Human genes 0.000 description 1
- 102100038945 Coiled-coil domain-containing protein 102A Human genes 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- 206010011732 Cyst Diseases 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- 101150021185 FGF gene Proteins 0.000 description 1
- 102100031706 Fibroblast growth factor 1 Human genes 0.000 description 1
- 102100024785 Fibroblast growth factor 2 Human genes 0.000 description 1
- 206010064571 Gene mutation Diseases 0.000 description 1
- 206010068601 Glioneuronal tumour Diseases 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- 102000009465 Growth Factor Receptors Human genes 0.000 description 1
- 108010009202 Growth Factor Receptors Proteins 0.000 description 1
- 102100029234 Histone-lysine N-methyltransferase NSD2 Human genes 0.000 description 1
- 101000613885 Homo sapiens BTB/POZ domain-containing protein KCTD1 Proteins 0.000 description 1
- 101000944500 Homo sapiens Cilia- and flagella-associated protein 58 Proteins 0.000 description 1
- 101000740818 Homo sapiens Coiled-coil domain-containing protein 102A Proteins 0.000 description 1
- 101000634048 Homo sapiens Histone-lysine N-methyltransferase NSD2 Proteins 0.000 description 1
- 101001006794 Homo sapiens Kinesin-like protein KIF6 Proteins 0.000 description 1
- 101001041393 Homo sapiens Serine protease HTRA1 Proteins 0.000 description 1
- 101000891623 Homo sapiens TBC1 domain family member 5 Proteins 0.000 description 1
- 101000891380 Homo sapiens Transcription elongation regulator 1-like protein Proteins 0.000 description 1
- 101000836154 Homo sapiens Transforming acidic coiled-coil-containing protein 1 Proteins 0.000 description 1
- 101000836148 Homo sapiens Transforming acidic coiled-coil-containing protein 2 Proteins 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 101150018316 Igsf3 gene Proteins 0.000 description 1
- 102100022519 Immunoglobulin superfamily member 3 Human genes 0.000 description 1
- 102100027927 Kinesin-like protein KIF6 Human genes 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 102000043276 Oncogene Human genes 0.000 description 1
- 108700020796 Oncogene Proteins 0.000 description 1
- 229940126233 Pemazyre Drugs 0.000 description 1
- 201000007288 Pleomorphic xanthoastrocytoma Diseases 0.000 description 1
- 102100021119 Serine protease HTRA1 Human genes 0.000 description 1
- 208000009574 Skin Appendage Carcinoma Diseases 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 229940125828 TAS-120 Drugs 0.000 description 1
- 102100040256 TBC1 domain family member 5 Human genes 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 102100040394 Transcription elongation regulator 1-like protein Human genes 0.000 description 1
- 102100027049 Transforming acidic coiled-coil-containing protein 1 Human genes 0.000 description 1
- 102100027044 Transforming acidic coiled-coil-containing protein 2 Human genes 0.000 description 1
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 description 1
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 description 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 210000002534 adenoid Anatomy 0.000 description 1
- 239000001361 adipic acid Substances 0.000 description 1
- 235000011037 adipic acid Nutrition 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 201000005781 adult medulloblastoma Diseases 0.000 description 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 210000003503 anal sac Anatomy 0.000 description 1
- 206010002224 anaplastic astrocytoma Diseases 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 235000010323 ascorbic acid Nutrition 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 229940092714 benzenesulfonic acid Drugs 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 239000003560 cancer drug Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 230000001364 causal effect Effects 0.000 description 1
- 230000024245 cell differentiation Effects 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 230000009134 cell regulation Effects 0.000 description 1
- 230000036755 cellular response Effects 0.000 description 1
- 208000019065 cervical carcinoma Diseases 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000011260 co-administration Methods 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- 208000031513 cyst Diseases 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 238000000113 differential scanning calorimetry Methods 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 229950005778 dovitinib Drugs 0.000 description 1
- 201000004428 dysembryoplastic neuroepithelial tumor Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000001678 elastic recoil detection analysis Methods 0.000 description 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000008622 extracellular signaling Effects 0.000 description 1
- 101150016624 fgfr1 gene Proteins 0.000 description 1
- 101150088071 fgfr2 gene Proteins 0.000 description 1
- 238000009093 first-line therapy Methods 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 230000012010 growth Effects 0.000 description 1
- 230000003862 health status Effects 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 150000003840 hydrochlorides Chemical group 0.000 description 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
- 229940071870 hydroiodic acid Drugs 0.000 description 1
- 230000001976 improved effect Effects 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 229950005712 infigratinib Drugs 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 229940045996 isethionic acid Drugs 0.000 description 1
- 230000000155 isotopic effect Effects 0.000 description 1
- 230000002147 killing effect Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229940099563 lactobionic acid Drugs 0.000 description 1
- 229950004231 lucitanib Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000005012 migration Effects 0.000 description 1
- 238000013508 migration Methods 0.000 description 1
- PSZYNBSKGUBXEH-UHFFFAOYSA-N naphthalene-1-sulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1 PSZYNBSKGUBXEH-UHFFFAOYSA-N 0.000 description 1
- 201000008026 nephroblastoma Diseases 0.000 description 1
- 238000007481 next generation sequencing Methods 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 206010073131 oligoastrocytoma Diseases 0.000 description 1
- 231100000590 oncogenic Toxicity 0.000 description 1
- 230000002246 oncogenic effect Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 230000003076 paracrine Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 229940121317 pemigatinib Drugs 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 102000054765 polymorphisms of proteins Human genes 0.000 description 1
- 238000000634 powder X-ray diffraction Methods 0.000 description 1
- 230000003449 preventive effect Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 125000004550 quinolin-6-yl group Chemical group N1=CC=CC2=CC(=CC=C12)* 0.000 description 1
- 230000008707 rearrangement Effects 0.000 description 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 description 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 description 1
- 238000004467 single crystal X-ray diffraction Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- 238000011269 treatment regimen Methods 0.000 description 1
- 229940116269 uric acid Drugs 0.000 description 1
- 229940005605 valeric acid Drugs 0.000 description 1
- 239000004474 valine Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 230000029663 wound healing Effects 0.000 description 1
- 238000002424 x-ray crystallography Methods 0.000 description 1
Images
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202163190602P | 2021-05-19 | 2021-05-19 | |
US63/190,602 | 2021-05-19 | ||
US202163242857P | 2021-09-10 | 2021-09-10 | |
US63/242,857 | 2021-09-10 | ||
US202163253316P | 2021-10-07 | 2021-10-07 | |
US63/253,316 | 2021-10-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
TW202313038A true TW202313038A (zh) | 2023-04-01 |
Family
ID=82067489
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TW111118772A TW202313038A (zh) | 2021-05-19 | 2022-05-19 | 用於治療晚期實性瘤之fgfr酪胺酸激酶抑制劑 |
Country Status (9)
Country | Link |
---|---|
EP (1) | EP4340840A1 (ja) |
JP (1) | JP2024518612A (ja) |
KR (1) | KR20240009465A (ja) |
AU (1) | AU2022277796A1 (ja) |
BR (1) | BR112023023935A2 (ja) |
CA (1) | CA3217517A1 (ja) |
MX (1) | MX2023013802A (ja) |
TW (1) | TW202313038A (ja) |
WO (1) | WO2022243467A1 (ja) |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4666828A (en) | 1984-08-15 | 1987-05-19 | The General Hospital Corporation | Test for Huntington's disease |
US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
US4801531A (en) | 1985-04-17 | 1989-01-31 | Biotechnology Research Partners, Ltd. | Apo AI/CIII genomic polymorphisms predictive of atherosclerosis |
US5272057A (en) | 1988-10-14 | 1993-12-21 | Georgetown University | Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase |
US5192659A (en) | 1989-08-25 | 1993-03-09 | Genetype Ag | Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes |
US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
CA2262403C (en) | 1995-07-31 | 2011-09-20 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
WO2006127926A2 (en) | 2005-05-23 | 2006-11-30 | Novartis Ag | Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one lactic acid salts |
US8163923B2 (en) | 2007-03-14 | 2012-04-24 | Advenchen Laboratories, Llc | Spiro substituted compounds as angiogenesis inhibitors |
GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
DK3125936T3 (da) * | 2014-03-31 | 2019-08-05 | Debiopharm Int Sa | Fgfr-fusioner |
LT3198033T (lt) * | 2014-09-26 | 2022-05-10 | Janssen Pharmaceutica Nv | Fgfr mutantinių genų rinkinių panaudojimas identifikuojant vėžiu sergančius pacientus, kurie reaguos į gydymą fgfr inhibitoriumi |
US20200208224A1 (en) * | 2014-09-26 | 2020-07-02 | Janssen Pharmaceutica Nv | Use Of FGFR Mutant Gene Panels In Identifying Cancer Patients That Will Be Responsive To Treatment With An FGFR Inhibitor |
EA202193276A1 (ru) * | 2019-05-28 | 2022-03-29 | Квед Терапьютикс, Инк. | Способы лечения холангиокарциномы |
-
2022
- 2022-05-19 JP JP2023571447A patent/JP2024518612A/ja active Pending
- 2022-05-19 TW TW111118772A patent/TW202313038A/zh unknown
- 2022-05-19 CA CA3217517A patent/CA3217517A1/en active Pending
- 2022-05-19 MX MX2023013802A patent/MX2023013802A/es unknown
- 2022-05-19 WO PCT/EP2022/063629 patent/WO2022243467A1/en active Application Filing
- 2022-05-19 KR KR1020237043394A patent/KR20240009465A/ko unknown
- 2022-05-19 EP EP22730734.5A patent/EP4340840A1/en active Pending
- 2022-05-19 AU AU2022277796A patent/AU2022277796A1/en active Pending
- 2022-05-19 BR BR112023023935A patent/BR112023023935A2/pt unknown
Also Published As
Publication number | Publication date |
---|---|
JP2024518612A (ja) | 2024-05-01 |
CA3217517A1 (en) | 2022-11-24 |
AU2022277796A1 (en) | 2024-01-18 |
KR20240009465A (ko) | 2024-01-22 |
BR112023023935A2 (pt) | 2024-01-30 |
WO2022243467A1 (en) | 2022-11-24 |
EP4340840A1 (en) | 2024-03-27 |
MX2023013802A (es) | 2023-12-06 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US11707463B2 (en) | FGFR2 inhibitors for the treatment of cholangiocarcinoma | |
TWI798199B (zh) | 癌症治療 | |
US20230110113A1 (en) | Fgfr tyrosine kinase inhibitors for the treatment of high-risk non-muscle invasive bladder cancer | |
US20220175768A1 (en) | Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma | |
CN117320724A (zh) | 用于治疗晚期实体瘤的fgfr酪氨酸激酶抑制剂 | |
TW202045173A (zh) | 癌症治療 | |
TW202313038A (zh) | 用於治療晚期實性瘤之fgfr酪胺酸激酶抑制劑 | |
JP2023542296A (ja) | Fgfr阻害剤の併用療法 | |
US20220054484A1 (en) | Fgfr tyrosine kinase inhibitors for the treatment of urothelial carcinoma | |
AU2018278271B2 (en) | FGFR2 inhibitors for the treatment of cholangiocarcinoma | |
US20240190858A1 (en) | Crystalline forms, pharmaceutical compositions and methods of use thereof | |
EP3852756A1 (en) | Treatment of cholangiocarcinoma |